Antimalarial preclinical drug development: A single oral dose of a 5-carbon-linked trioxane dimer plus mefloquine cures malaria-infected mice

Deuk Kyu Moon, Vandana Singhal, Nirbhay Kumar, Theresa A Shapiro, Gary H. Posner

Research output: Contribution to journalArticle

Abstract

Three new 5-carbon-linked trioxane dimer carboxylate esters have been prepared from the natural trioxane, artemisinin, in only three steps and 40-50% overall yields. Each one of these new chemical entities is at least as efficacious as the clinically used trioxane antimalarial drug artemether when combined with mefloquine hydrochloride in a low single oral dose cure.

Original languageEnglish (US)
Pages (from-to)76-81
Number of pages6
JournalDrug Development Research
Volume71
Issue number1
DOIs
StatePublished - Feb 2010

Fingerprint

Mefloquine
Antimalarials
Malaria
Esters
Carbon
artemisinine
artemether

Keywords

  • Antimalarial chemotherapy
  • Artemisinin combination therapy (ACT)
  • Single oral dose ACT cure
  • Trioxane dimers

ASJC Scopus subject areas

  • Drug Discovery

Cite this

Antimalarial preclinical drug development : A single oral dose of a 5-carbon-linked trioxane dimer plus mefloquine cures malaria-infected mice. / Moon, Deuk Kyu; Singhal, Vandana; Kumar, Nirbhay; Shapiro, Theresa A; Posner, Gary H.

In: Drug Development Research, Vol. 71, No. 1, 02.2010, p. 76-81.

Research output: Contribution to journalArticle

@article{f499797abd0a40dfbe3c282e2c5af742,
title = "Antimalarial preclinical drug development: A single oral dose of a 5-carbon-linked trioxane dimer plus mefloquine cures malaria-infected mice",
abstract = "Three new 5-carbon-linked trioxane dimer carboxylate esters have been prepared from the natural trioxane, artemisinin, in only three steps and 40-50{\%} overall yields. Each one of these new chemical entities is at least as efficacious as the clinically used trioxane antimalarial drug artemether when combined with mefloquine hydrochloride in a low single oral dose cure.",
keywords = "Antimalarial chemotherapy, Artemisinin combination therapy (ACT), Single oral dose ACT cure, Trioxane dimers",
author = "Moon, {Deuk Kyu} and Vandana Singhal and Nirbhay Kumar and Shapiro, {Theresa A} and Posner, {Gary H.}",
year = "2010",
month = "2",
doi = "10.1002/ddr.20350",
language = "English (US)",
volume = "71",
pages = "76--81",
journal = "Drug Development Research",
issn = "0272-4391",
publisher = "John Wiley and Sons Inc.",
number = "1",

}

TY - JOUR

T1 - Antimalarial preclinical drug development

T2 - A single oral dose of a 5-carbon-linked trioxane dimer plus mefloquine cures malaria-infected mice

AU - Moon, Deuk Kyu

AU - Singhal, Vandana

AU - Kumar, Nirbhay

AU - Shapiro, Theresa A

AU - Posner, Gary H.

PY - 2010/2

Y1 - 2010/2

N2 - Three new 5-carbon-linked trioxane dimer carboxylate esters have been prepared from the natural trioxane, artemisinin, in only three steps and 40-50% overall yields. Each one of these new chemical entities is at least as efficacious as the clinically used trioxane antimalarial drug artemether when combined with mefloquine hydrochloride in a low single oral dose cure.

AB - Three new 5-carbon-linked trioxane dimer carboxylate esters have been prepared from the natural trioxane, artemisinin, in only three steps and 40-50% overall yields. Each one of these new chemical entities is at least as efficacious as the clinically used trioxane antimalarial drug artemether when combined with mefloquine hydrochloride in a low single oral dose cure.

KW - Antimalarial chemotherapy

KW - Artemisinin combination therapy (ACT)

KW - Single oral dose ACT cure

KW - Trioxane dimers

UR - http://www.scopus.com/inward/record.url?scp=76749103780&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=76749103780&partnerID=8YFLogxK

U2 - 10.1002/ddr.20350

DO - 10.1002/ddr.20350

M3 - Article

AN - SCOPUS:76749103780

VL - 71

SP - 76

EP - 81

JO - Drug Development Research

JF - Drug Development Research

SN - 0272-4391

IS - 1

ER -